Professional Documents
Culture Documents
Alka Oli Des
Alka Oli Des
Gymnosperms
Rarely contain Alkaloids like Taxaceae family
Occurrence of Alkaloids:
Alkaloids occur in,
Seeds Physostigma, Areca
Fruits Conium
Leaves Belladonna, Coca
Underground stem Sangunaria
Roots Belldonna
Roots and rhizomes Ipecac, Hydrastis
Barks cinchonna
Fungi Ergot
Taxonomy of Alkaloids:
They can be named on basis of,
Genus name of plant Hydrastine, Atropine
Species name of plant Cocaine,
belladonine
Common name of plant Ergotamine
Pharmacological activity Emetine,
Morphine
Ocassionally on the name of discoverer
Ajmaline, Pelletiernine
Properties of Alkaloids:
Alkaloids usually contain 1 Nitrogen atom.
Some may contain up to 5 nitrogen atoms.
Nitrogen may exist as;
1. Primary amine R – NH2
2. Secondary amine R2 – NH
3. Tertiary amine R3 – N
4. Quaternary amine R4 – N+X-
Physical properties:
The various physical properties are;
Alkaloids are usually bitter in taste
Alkaloids are insoluble or sparingly soluble in
water., but alkaloidal salts are freely soluble in water
Free Alkaloids are usually soluble in ether,
chloroform and other relatively non polar solvents.
Most of the alkaloids are crystalline solids, few
Alkaloids are amorphous
Some are liquids (usually which lack oxygen) like
Nicotine, Conine and sarpenteine.
Alkaloidal salts are also crystalline in nature
Role of Alkaloids in Plants:
In plants alkaloids performs various functions
given below;
Poisonous agents protecting plants against
insect and herbivores attack
End products of detoxification reactions, so are
metabolic locking-up of compounds harmful to
plants
Regulatory factors
Reserve substances for supplying Nitrogen and
other elements to plants
Like many other secondary metabolic products
Pharmacological activities of Alkaloids
Alkaloids are capable of extensive pharmacological
activity and display variety of pharmacological actions
like Alkaloids are,
1. Analgesics and Norcotics Morphine, Codeine
2. Central NS Stimulants Strychnine, Brucine
3. Mydriatics Atropine
4. Myotics Physostigmine, Pilocarpine
5. Hypertenssives Ephedrine
6. Antihypertenssives Reserpine
7. Anti malarials Quinine
8. Antiarrhythmic Quinidine
9. Oxytocic agent Methyl Ergonovine
Classification of Alkaloids
Alkaloids are generally classified by;
Their molecular precursors, based on the
biological pathway used to construct the
molecule. From Structural point of view, alkaloids
are divided according to their shape and origins.
Alkaloids are classified in three main types,
1. True Alkaloids Derived from Amino acids
2. Proto Alkaloids Derived from Amino acids
3. Pseudo Alkaloids Not derived from Amino
acids
1. True Alkaloids:
These are derived from Amino acids. They share
heterocyclic ring with Nitrogen. They are highly
reactive substances with biological activity at low
doses. Most of the alkaloids belongs to this group.
They occur in plants,
1. In Free State
2. As salts
3. As N-oxides
Drugs: Cinchona
4. Isoquinoline Alkaloids
Drugs: Pilocarpus
7. Steroidal Alkaloids
Drugs: Veratrum
8. Alkaloidal Amines
(i) Ipecac
Botanical origin: Cephaelis ipecacuanha,
Cephaelis acuminata
Family: Rubiaceae
Part used: Dried Roots and Rhizomes
Habitat:
It is mainly cultivated in Brazil. Brazil is also a
major exporter of the drug. Some cultivation is
also carried out in Malaysia and India.
Constituents:
It contain isoquinoline alkaloids. The major
alkaloids are emetine, cepheline and
psychotrine.
Medicinal uses:
- It is used as emetic. Ipecac syrup is
available in market which is used for this
purpose.
Common name: Post, Afim
Botanical origin: Papaver somniferum
Family: Papveraceae
Part used:
Dried milky latex obtained by the incision of
fully grown but unripe capsules.
Habit: Annual herb
Habitat:
The drug is cultivated in India, Persia,
Macedonia, Turkey, China, Afghanistan and
Pakistan.
It is cultivated in October with selective seeds. After
growth of about 2cm to 3cm plant out, winter season
starts at that time growth retarded. In spring season,
it grows little. When seedlings are of 12cm to 14cm,
thinning of seeds are done. Flowers occur in June and
July. Purple white or yellow flower and poppy start
growing on each plant.
When capsule start maturing from purple to yellow
the constituents are at its peak. Cuts are applied so
that endocarp don’t get damage. Latex oozes out,
initially it is white but on exposure to sun and it turns
brown.
Latex is converted into kneaded into small box and
packed in opium leaves and is shade dried and these
balls are crude opium.
Constituents:
Over 30 different alkaloids have been derived
from opium. Major alkaloids are morphine 4% -
21%, thebaine, noscapine, codeine, codinone
0.8% - 2.5%, papaverine and protopine.
There are three varieties of opium which are
commercially available;
Indian opium, previously it was considered
good but not now available in markets.
Chinese opium, it is of best quality.
Turkish opium
Medicinal uses:
- It acts on CNS initially a stimulant action
but then a depressant action of them.
- These are potent analgesics.
- Especially they are used in Cancer induced
pains.
- One of the major back draw of these drugs
is addiction.
- They are used to treat cough especially
codeine, an ingredient of cough syrups.
A number of theraputic drugs belongs to this
class. The drugs of this class are;
1. Nux-vomica (strychnine, brucine)
2. Rauwolfia (serpentine, ajmaline)
3. Catharanthus (vincristine, vinblastine)
4. Ergot (ergotine, ergotamine)
5. Physostigma (physistigmine)
Common name: Snake root
Botanical origin: Rauwolifia serpentina
Family: Apocynaceae
Part used: Dried roots but sometimes rhizomes
and stem cuttings are also used.
Habit: It is 1 meter tall erect shrub with wiry
roots
Habitat:
It is found in India, Burma, Sri-Lanka, Vietnam,
Malaysia, Indonesia, and Philippines. It is also
present in the hot climates of the world. Major
supplies are form India and Thiland.
Constituents:
Over 50 different alkaloids have been isolated,
major are reserpine, serpentine, resepinine,
ajmaline, and isoajmaline.
Medicinal uses:
- It is used as hypotensive sedative agent.
Especially, reserpine is antihypertensive agent. It
slows down the pulse rate and produce euphoria.
- It is used to treat cardiac arrhythmia.
- It is used as hypnotic agent.
- It is used to treat neuro-psychotic disorders.
Botanical origin: Vinca rosea, Catharanthus
roseus
Family: Apocynaceae
Part used: Dried whole plant parts
Habitat: It is native to Madagascar but it is
cultivated as ornamental plant cell over the
world in tropical areas.
Constituents: It contain indol-indolene alkaloids in it.
The major alkaloids are vinblastine, vincristine,
venerosine and extra. Vincristine and vinblastine are
unstable and need refrigeration 0oC – 8oC.
Medicinal uses:
- It is used to treat various cancers.
- Vinblastine sulphate used to treat ovarian cancer, it
is resistant to other therapies.
- Vinblastine is also used to treat Hodgkin’s disease.
- Vincristine sulphate is used in combination with
anticancer agents to treat Hodgkin’s disease.
- Vincristine is also used to treat leukemia.
(iii) Nux-vomica
Botanical origin: Strychnos nuxvomica
Family: Loganiaceae
Part used: Dried ripe seeds
Habitat It is found in Africa and Sri Lanka.
Constituents:
It contain different alkaloids. The major
alkaloids are brucine, loganine, Strychnine.
The total alkaloidal content is about 3% to 5%.
Strychnine constitute 1/3rd of total alkaloids.
Strychnine is major alkaloid and is more
pharmacologically active. It is present in the
thick walled endospermic cells present in the
center of the cell. While, brucine is present in
the outer part of the seeds.
Medicinal uses:
- They are not currently employed in the
medicine but are used in neuroanatomical
research.
- These are CNS stimulants.
- It is used as Pesticides specially to kill
rodents.
- Strychnine is more toxic than brucine it is
used for alcohol denaturing.
- It is used as tonic for sexual impotence.
- It is used to produce paralysis of intestine.
Botanical origin: Physostigma venenosum
Family: Leguminosae
Part used: Dried Ripe seeds
Habitat:
It is found in West Africa and in the vicinity of
gulf of Guinea. Plant contains poisnous
alkaloides.
Constituents:
It contain contain alkaloids. The total
alkaloidal content is 0.15%. The major
alkaloids are physostigmine (serine),
physovenine, esramine, and genesine.
Medicinal uses:
- They are used as a reversible inhibitors of
choline esterase.
- 0.25% ointment of physostigmine is used
topically on conjunctiva 3 to 4 times a day.
- Physostigmine potentiated the effects of
Acetyl choline.
- It is used as antidote for anticholinergic
inhibitors.
Botanical origin: Secale cereale
Family: Graminae
Part used: Dried sclerotium developed on rye
plant
Habitat: It is found in Yugoslavia, Switzerland,
Hungary, and Czechoslovakia.
Collection: The ergot is formed by the fungus
Cleviceps purourea (Clavicipitaceae or
Hypocreaceae).
Asexual stage:
In spring season one of the fungal spore come in contact
with rye plant. It resides over the ovary. Hyphal strands are
produced which penetrate into the ovary for nutrition.
Fungus is parasitic in nature. Hyphal strands will
eventually from a soft white mass called mycelium. Some
of the hyphal strands in mycelium will produce asexual
spore called conidiospores. These conidiospores will be
suspended in honey dew (a secretary secretion of
mycelium). Insects will be attracted to honey dew.
Conidiospore than will be carried to another host plant
through the insect to repeat the cycle. This stage of
development is called asexual or Sphacelial stage.
Sexual stage:
In this stage of development the mycelium grown
in size and eventually replace entire ovary to
form soft white color mass which over the time
will become hard and purple in color to form
Seclerotia. These seclerotia will fall down on
ground over the winter season.
In the start of spring season sexual spores will be
produced in seclerotium and will repeat the
entire cycle. This stage of development is called
sexual or Ascigerous cycle.
Constituents:
It contain indole alkaloids more specifically
ergot alkaloids are derivatives of Lysergic acid
LSD. The total alkaloidal content is 0.15%.
The major alkaloids are ergotmine and its
isomer ergotaminine, ergonovine, erginine,
methyl ergonovine.
Medicinal uses:
- It is used as oxytocic agent (increase
uterine muscle contractions), these include
strong uterine muscle contraction.
- It is used in labour room to facilitate the
baby birth.
- It also help to prevent post-partum
haemorrhage.
- It is used to treat migraine. They produce
vasodilation and decrease blood pressure.
These alkaloids contain imidazole ring in their
chemical structure. The class includes Pilocarpus.
(i) Pilocarpus
Botanical origin:
Veratrum viridi
Veratrum album
Family: Liliaceae
Part used:
Dried rhizomes and roots
Dried rhizome
Habit: Shrub
Constituents:
These alkaloids have cholesterol like structure. Basic ring
is present in such alkaloids is perhydrocyclopentano
phenantherine ring.
There different types of alkaloids are present in Veratrum
viridi are;
Group 1: esters of alkamine with organic acids. For
example; Cevadine, Germidine, Germitrine, Neogermitrine,
Protoveratrine A and Veratrine.
Group 2: glucoalkaloids or glucoalkamines. For example;
pseudojervine and veratrosine.
Group 3: alkamines. For example; Germine, rubijervine
and jervine.
Family: Gnetaceae
Part used: Whole herb
Habitat:
It is indigenous to the China, also found in India,
Pakistan, Indonesia, and Spain. Plants usually
grows in sandy clay soil. It has been used in
medicine since 5000 years especially in Chinese
medicine system.
Constituents:
It contain Ephedrine, which is alkaloidal amine
and is biosynthesized from phenyl alanine amino
acid. Ephedrine is therapeutically active
compound. Pseudoephedrine is also present in
plant to a lesser extent.
Uses:
Ephedrine HCl and Ephedrine SO4 used therapeutically.
Both these drugs are soluble in water and in hot alcohol
but are soluble in ether.
- Ephedrine HCl is sympathomimetic drug. It increases the
blood pressure.
- It is a CNS stimulant.
- Ephedrine SO4 is used as vasoconstrictor and
bronchodilator.
- Both these salts are used to treat asthma and hay fever.
- Ephedrine and pseudoephedrine are used in cough syrup
as antitussive agent.
- Ephedrine is a cardio stimulant drug.
- It is a potent vasoconstrictor.
They are also known as purine lakloids.
Purine ring is formed of two rings.
Pyrimidine ring
Imidazole ring
The class includes only two drugs;
Coffee
Tea
(i) Coffee
Botanical origin: Coffea arabica
Family: Rubiaceae
Part used: Dried roasted seeds/ beans
Habit: Shrub
Habitat:
Coffee is from Turkish word or Arabic word ‘quveh’ or
‘quhah’. Arabica shows the habitat. It is indigenous to
Ethiopia and Eastern Africa. It is also cultivated world over
in Tropical countries mainly in Indonesia, Sri Lanka,
Central & Southern America and Brazil. Brazil is the major
producer. It produces 600,000 tons of coffee. The yield of
coffee is 0.5kg – 5kg per plant.
Constituents:
Tea contain xanthine derivatives. Caffeine (1,
3, 7-trimethyl xanthine), theophylline (1, 3-
dimethyl xanthine), tannins (gallotannic acid),
Theobromine (1, 7-dimethyl xanthine),
proteins and volatile oils. Aroma is due to
volatile oil.
Uses:
The usual cup of tea contain 60mg of caffeine in it.
- Caffeine is CNS stimulant.
- Caffeine is used as stimulent of cardiac and respiratory
center.
- Caffeine also acts in smooth muscles and kidneys.
- Tea is astringent due to tannins.
- Theophylline is smooth muscle relaxant.
- Theophylline is used as bronchodilator in asthma.
- Theophylline is used as diuretic in cardiac patients.
- Theobromine is also used as smooth muscle relaxant
and diuretic but it is ppreferred over theophylline because
it doesn’t act of CNS system as theophylline.
- It is preferred in patients having Chronic heart failure of
angina.